biostudies-literatureRavish ANational Research Foundation of Korea (NRF)DBT-NER, and Vision Group on Science and Technology (CESEM), Government of KarnatakaShenzhen Key Laboratory of Innovative OncotherapeuticsResearchers Supporting ProjectOverseas Research Cooperation ProjectShenzhen Development and Reform Commission Subject Construction ProjectTsinghua University Stable Funding Key ProjectShenzhen Bay Laboratory159https://www.ebi.ac.uk/biostudies/studies/S-EPMC9952374biostudies-literatureUnknown10(2)In breast cancer (BC), STAT3 is hyperactivated. This study explored the design of imidazopyridine-tethered pyrazolines as a de novo drug strategy for inhibiting STAT3 phosphorylation in human BC cells. This involved the synthesis and characterization of two series of compounds namely, 1-(3-(2,6-dimethylimidazo [1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-(4-(substituted)piperazin-1-yl)ethanone and N-substituted-3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazoline-1-carbothioamides. Compound <b>3f</b> with 2,3-dichlorophenyl substitution was recognized among the tested series as a lead structure that inhibited the viability of MCF-7 cells with an IC₅₀ value of 9.2 μM. A dose- and time-dependent inhibition of STAT3 phosphoBioengineering (Basel, Switzerland)De Novo Design of Imidazopyridine-Tethered Pyrazolines That Target Phosphorylation of STAT3 in Human Breast Cancer Cells.PMC9952374[2017]1434HW2020008NRF-2021R1I1A206002421310031RSP2023R5WDZC20200821150704001ZDSYS20200820165400003Alharbi SAXi ZLobie PEYang JRShivakumar RChinnathambi ARavish ASwamynayaka APandey VBasappa BMadegowda MYang MHAhn KSNagaraja OSethi GfalseDe Novo Design of Imidazopyridine-Tethered Pyrazolines That Target Phosphorylation of STAT3 in Human Breast Cancer Cells.In breast cancer (BC), STAT3 is hyperactivated. This study explored the design of imidazopyridine-tethered pyrazolines as a de novo drug strategy for inhibiting STAT3 phosphorylation in human BC cells. This involved the synthesis and characterization of two series of compounds namely, 1-(3-(2,6-dimethylimidazo [1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-(4-(substituted)piperazin-1-yl)ethanone and N-substituted-3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazoline-1-carbothioamides. Compound <b>3f</b> with 2,3-dichlorophenyl substitution was recognized among the tested series as a lead structure that inhibited the viability of MCF-7 cells with an IC₅₀ value of 9.2 μM. A dose- and time-dependent inhibition of STAT3 phospho2023-01-01T00:00:00Z2023 Jan2026-04-08T13:21:42.807Z2025-02-19T00:14:00.673ZS-EPMC99523743682965310.3390/bioengineering10020159